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单胺类物质作为巴氯芬抗伤害感受作用的介质。

Monoamines as mediators of the antinociceptive effect of baclofen.

作者信息

Sawynok J

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(1):54-7. doi: 10.1007/BF00498828.

Abstract

The antinociceptive activity of baclofen was evaluated in rats using the tail flick and hot plate tests. When baclofen was administered intraperitoneally, pretreatment with depletors of monoamines and catecholamines (reserpine, alpha-MPT) produced a marked increase in antinociceptive activity in both tests. Blockade of noradrenergic and dopaminergic receptors with phentolamine, chlorpromazine and haloperidol produced similar increases. These agents were without intrinsic effect in these tests except for alpha-MPT which increased the tail flick latency slightly. Alterations in serotonergic function did not consistently alter the action of baclofen. When baclofen was administered intrathecally, pretreatment with reserpine and alpha-MPT produced minimal alterations in antinociceptive activity. It is likely that interactions between baclofen and monoamines occur at supraspinal sites.

摘要

使用甩尾试验和热板试验在大鼠中评估了巴氯芬的抗伤害感受活性。当腹腔注射巴氯芬时,用单胺和儿茶酚胺耗竭剂(利血平、α-甲基对酪氨酸)预处理在两种试验中均使抗伤害感受活性显著增加。用酚妥拉明、氯丙嗪和氟哌啶醇阻断去甲肾上腺素能和多巴胺能受体会产生类似的增加。除α-甲基对酪氨酸使甩尾潜伏期略有增加外,这些药物在这些试验中无内在作用。5-羟色胺能功能的改变并未持续改变巴氯芬的作用。当鞘内注射巴氯芬时,用利血平和α-甲基对酪氨酸预处理对抗伤害感受活性产生的改变极小。巴氯芬与单胺之间的相互作用可能发生在脊髓上部位。

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